Affiliation: | 1. Institute of Medical Science, University of Toronto, 1 Kings College Circle, Toronto, ON M5S 1A8 Canada Azrieli Centre for Neuro-Radiochemistry, Brain Health Imaging Centre, Centre for Addiction and Mental Health (CAMH), 250 College Street, Toronto, ON M5T 1R8 Canada;2. Azrieli Centre for Neuro-Radiochemistry, Brain Health Imaging Centre, Centre for Addiction and Mental Health (CAMH), 250 College Street, Toronto, ON M5T 1R8 Canada;3. Department of Radiology and Imaging Sciences, Emory University, Atlanta, GA, 30322 USA;4. Institute of Medical Science, University of Toronto, 1 Kings College Circle, Toronto, ON M5S 1A8 Canada |
Abstract: | Positron emission tomography (PET) is a powerful imaging tool for drug discovery, clinical diagnosis, and monitoring of disease progression. Fluorine-18 is the most common radionuclide used for PET, but advances in radiotracer development have been limited by the historical lack of methodologies and precursors amenable to radiolabeling with fluorine-18. Radiolabeling of electron-rich (hetero)aromatic rings remains a long-standing challenge in the production of PET radiopharmaceuticals. In this personal account, we discuss the history of spirocyclic iodonium ylide precursors, from inception to applications in clinical research, for the incorporation of fluorine-18 into complex non-activated (hetero)aromatic rings. |